Chrysin, baicalein and galangin are indirect activators of the human constitutive androstane receptor (CAR)

Result code in IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61989592%3A15310%2F15%3A33153848" target="_blank" >RIV/61989592:15310/15:33153848 - isvavai.cz</a>

Alternative codes found

RIV/00216208:11160/15:10312776

Result on the web

<a href="http://www.sciencedirect.com/science/article/pii/S0378427415000259" target="_blank" >http://www.sciencedirect.com/science/article/pii/S0378427415000259</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1016/j.toxlet.2015.01.013" target="_blank" >10.1016/j.toxlet.2015.01.013</a>

Result language

angličtina

Original language name

Chrysin, baicalein and galangin are indirect activators of the human constitutive androstane receptor (CAR)

Original language description

The constitutive androstane receptor (CAR) is a crucial transcriptional regulator of key xenobiotic-metabolizing enzymes such as cytochrome P450 CYP3A4, CYP2C9 and CYP2B6. The flavonoids chrysin, baicalein and galangin have been reported to activate CARand interfere with EGFR signaling. Nevertheless, it is not known if these flavonoids are direct CAR ligands or indirect phenobarbital-like CAR activators via the inhibition of epidermal growth factor receptor (EGFR) signaling. We analyze the interactionsof chrysin, galangin and baicalein and its glycoside baicalin with human CAR. We have employed and validated methods that can study direct interaction with the CAR ligand binding pocket. Secondly, we determined if the compounds affect human EGFR signaling and interact with EGFR. Employing a TR-FRET coactivator assay with recombinant CAR or CAR assembly assay, a consistent activation of CAR with flavonoids and phenobarbital was not observed. It was determined, however, that galangin, chr

Czech name

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Czech description

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Type

J_x - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)

CEP classification

FR - Pharmacology and apothecary chemistry

OECD FORD branch

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Project

<a href="/en/project/GBP303%2F12%2FG163" target="_blank" >GBP303/12/G163: Centre of drug-dietary supplements interactions and nutrigenetics</a><br>

Continuities

P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)

Publication year

2015

Confidentiality

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Name of the periodical

Toxicology Letters

ISSN

0378-4274

e-ISSN

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Volume of the periodical

233

Issue of the periodical within the volume

2

Country of publishing house

IE - IRELAND

Number of pages

10

Pages from-to

68-77

UT code for WoS article

000349631300002

EID of the result in the Scopus database

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